Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure–activity–relationship, and sleep-promoting properties in rats

Abstract

Medicinal chemistry efforts starting from the GPCR agonist HTS hit 1 led to the discovery of the potent, selective, brain-penetrating, orally active orexin 2 receptor antagonists 43 that induced sleep in rats.